{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["1(9)"],"submitter":["Jin M"],"pubmed_abstract":["This report describes the investigation of a series of 5,7-disubstituted imidazo[5,1-f][1,2,4]triazine inhibitors of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR). Structure-activity relationship exploration and optimization leading to the identification, characterization, and pharmacological activity of compound 9b, a potent, selective, well-tolerated, and orally bioavailable dual inhibitor of IGF-1R and IR with in vivo efficacy in tumor xenograft models, is discussed."],"journal":["ACS medicinal chemistry letters"],"pagination":["510-5"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC4007908"],"repository":["biostudies-literature"],"pubmed_title":["Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR."],"pmcid":["PMC4007908"],"pubmed_authors":["Laufer RS","Kleinberg A","Cooke A","Gokhale PC","Mulvihill MJ","Stolz KM","Foreman K","Werner DS","Landfair D","Feng L","Siu KW","Yao Y","Wild R","Bittner MA","Li AH","Dong H","Jin M","Steinig AG","Kadalbajoo M","May EW","Buck E","Pachter JA"],"additional_accession":[]},"is_claimable":false,"name":"Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR.","description":"This report describes the investigation of a series of 5,7-disubstituted imidazo[5,1-f][1,2,4]triazine inhibitors of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR). Structure-activity relationship exploration and optimization leading to the identification, characterization, and pharmacological activity of compound 9b, a potent, selective, well-tolerated, and orally bioavailable dual inhibitor of IGF-1R and IR with in vivo efficacy in tumor xenograft models, is discussed.","dates":{"release":"2010-01-01T00:00:00Z","publication":"2010 Dec","modification":"2025-04-05T10:37:36.761Z","creation":"2019-03-27T01:27:30Z"},"accession":"S-EPMC4007908","cross_references":{"pubmed":["24900240"],"doi":["10.1021/ml100178g"]}}